Compound Monograph

Kaempferitrin

Phenolics Flavonols Natural (plant-derived)

Kaempferitrin is kaempferol-3,7-O-α-L-dirhamnoside (synonym lespedin) — a flavonol diglycoside of epazote, Justicia and many plants. No human trial of the isolate exists; its evidence is a small preclinical set led by a genuine insulin-mimetic antidiabetic signal (it stimulates glucose uptake in skeletal muscle and is hypoglycemic in diabetic rodents), with anti-inflammatory and antioxidant data. Poorly absorbed and hydrolyzed toward kaempferol in the gut.

Sources · 5

Where Does It Come From?

Kaempferitrin is a naturally occurring flavonol glycoside (kaempferol-3,7-o-α-l-dirhamnoside), found in Epazote and 4 other sources. It is well tolerated orally (low toxicity).

Also found in
Bauhinia forficata Monograph coming soon
Justicia spicigera Monograph coming soon
Kenaf Monograph coming soon
Sedum dendroideum Monograph coming soon

Concentration

Content by Source

Concentrations not reported. No percent-dry-weight or mg/g figures have been published for this compound in its source plants.

Kaempferitrin at a Glance

Kaempferitrin is kaempferol-3,7-O-alpha-L-dirhamnoside — a flavonol diglycoside of epazote, Justicia and many other plants, also known as lespedin.

Its evidence is a small preclinical set led by a genuinely notable finding: insulin-like hypoglycaemic activity, reported to lower blood glucose in diabetic animals with a rapidity more typical of a hormone than a flavonoid.

No human trial of the isolate exists.

What It's Used For

Kaempferitrin is the 3,7-dirhamnoside of kaempferol (synonym lespedin, an identity established in 1951 13Reference 13HATTORI S · 1951Identity of lespedin with kaempferitrinView study →) — a sibling of the monoglucoside astragalin, from which it differs by carrying a second (7-position) sugar and swapping glucose for rhamnose (twice). Its evidence is a small, multi-lab preclinical literature clustered on one genuinely distinctive signal: an insulin-mimetic antidiabetic effect. Unlike most flavonol glycosides, kaempferitrin shows an intact-molecule action in muscle — so it is not purely a kaempferol prodrug — although its poor absorption and gut-flora hydrolysis toward kaempferol still make chronic oral benefit bioavailability-limited. No human trials of the isolate exist.

A genuine, somewhat kaempferitrin-specific antidiabetic signal:the intact molecule stimulates glucose uptake in skeletal muscle and adipocyte insulin signaling, and is hypoglycemic in diabetic rodents 1,3,2Reference 1Jorge AP et al. · 2004AnimalInsulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscleView study →Reference 3Tzeng YM et al. · 2009Kaempferitrin activates the insulin signalling pathway and stimulates secretion of adiponectin in 3T3-L1 adipocytesView study →Reference 2de Sousa E et al. · 2004Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leavesView study →.
The honest headline:no human trials; the glucose-uptake data are tissue-divergent (muscle up, one adipocyte study down), and the anti-inflammatory/antioxidant signals are largely shared with the kaempferol class 4Reference 4Vishnu Prasad CN et al. · 2009Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytesView study →.
Evidence by IndicationStrength of support · Beta

Support is an experimental score — weighted by study type (human > animal > in vitro) and volume. A beta, not a validated metric. No human isolate data, so scores stay low by design.

Mechanisms

Target / pathwayEffectRelevant to
Skeletal-muscle glucose uptake (insulin-mimetic)↑ uptake, insulin-signaling-dependent
antidiabetic
Insulin signaling (IR → PI3K/Akt) + adiponectinpathway activated; ↑ adiponectin
antidiabetic
GLUT4 translocationtissue-divergent — muscle uptake up, but inhibited in one adipocyte study
antidiabetic (nuance/contradiction)
Hepatic AMPK / PEPCK↑ AMPK, ↓ PEPCK → ↓ gluconeogenesis
antidiabetic (in vivo)
NF-κB; NOX4 → tubular ferroptosissuppressed; inhibited
anti-inflammatory / antioxidant
ROS / AGE-induced oxidative stressreduced
diabetic-complication protection
Intrinsic (mitochondrial) apoptosispro-apoptotic in tumor cells
antitumor

Pharmacokinetics

No dedicated human pharmacokinetics exists. As a flavonol 3,7-di-O-rhamnoside, kaempferitrin is a poorly absorbed, high-polarity diglycoside: the two rhamnose units block passive uptake, and human intestinal flora biotransform it by stepwize deglycosylation (loss of rhamnose → monorhamnoside intermediates → the aglycone kaempferol), which is then conjugated 12Reference 12Yang XW et al. · 2005The biotransformation of kaempferitrin by human intestinal floraView study →. The net result is low, non-sustained systemic exposure to the intact parent, and a meaningful fraction of chronic in-vivo activity should be read as kaempferol-equivalent exposure (see kaempferol). The important nuance: the acute insulin-mimetic muscle effects are reported for the intact molecule in ex-vivo/cell systems, so the antidiabetic mechanism is not purely a kaempferol proxy — but oral, whole-animal benefit is bioavailability-limited.

Clinical trials

There are no randomized or open-label human trials of isolated kaempferitrin for any indication; human relevance is limited to dietary/traditional intake within kaempferitrin-bearing plants (epazote, Justicia spicigera, Bauhinia forficata).

CompletedPlannedTerminatedPreclinical
—(none, isolate)——Small multi-lab set (antidiabetic-led)

Last checked: July 2026.

Toxicity & Safety

Kaempferitrin is a dietary flavonol glycoside with no harm signal at food levels, and the only caution with a real mechanism behind it is the mirror image of its main effect — its glucose-lowering activity could add to antidiabetic medication.

Safety at a Glance
Low / no toxicityDrug interactionsBleeding risk
  • A dietary flavonol with no harm signal. Used across preclinical studies as a protective agent; one extract study reported antitumor efficacy without hepatotoxicity.
  • Avoid isolated supplements in pregnancy and lactation. Dietary amounts are a separate question.
  • Possible additive hypoglycemia. The insulin-mimetic signal makes stacking with antidiabetic drugs plausible in theory, though unquantified in humans.
  • Generic polyphenol-supplement caution. Possible additive effects with antiplatelet or anticoagulant therapy.
  • No isolate toxicology. No genotoxicity or human safety dataset exists for the purified compound.
Full Safety & Interactions Detail

Kaempferitrin is a dietary flavonol glycoside in food and medicinal plants, used across preclinical studies as a protective or benign agent with no dietary harm signal — consistent with a low flag; notably, the epazote-extract xenograft study reported antitumor efficacy without hepatotoxicity 11Reference 11Su M et al. · 2023AnimalKaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenograftsView study →.

There is no isolate toxicology, genotoxicity or human safety dataset, and cautions are theoretical and generic to concentrated polyphenol supplements (possible additive effects with antiplatelet/anticoagulant therapy). One specific pharmacodynamic caution: given the insulin-mimetic/glucose-lowering signal, additive hypoglycemia with antidiabetic drugs is plausible in theory though unquantified in humans.

Dosage

There is no efficacy dose established (no human trials) and no standard supplemental dose — kaempferitrin is obtained incidentally through diet and herbal preparations rather than dosed on its own, and any oral efficacy target is undercut by its poor absorption and gut-flora hydrolysis to kaempferol, so a meaningful “kaempferitrin dose” cannot honestly be stated.

References

  1. Jorge AP, Horst H, de Sousa E, et al. (2004). Insulinomimetic effects of kaempferitrin on glycaemia and on ¹⁴C-glucose uptake in rat soleus muscle. Chemico-Biological Interactions. https://pubmed.ncbi.nlm.nih.gov/15501431/
  2. de Sousa E, Zanatta L, Seifriz I, et al. (2004). Hypoglycemic effect and antioxidant potential of kaempferol-3,7-O-(α)-dirhamnoside from Bauhinia forficata leaves. Journal of Natural Products. https://pubmed.ncbi.nlm.nih.gov/15165145/
  3. Tzeng YM, Chen K, Rao YK, et al. (2009). Kaempferitrin activates the insulin signalling pathway and stimulates secretion of adiponectin in 3T3-L1 adipocytes. European Journal of Pharmacology. https://pubmed.ncbi.nlm.nih.gov/19326566/
  4. Vishnu Prasad CN, Suma Mohan S, Banerji A, et al. (2009). Kaempferitrin inhibits GLUT4 translocation and glucose uptake in 3T3-L1 adipocytes. Biochemical and Biophysical Research Communications. https://pubmed.ncbi.nlm.nih.gov/19146827/
  5. Cazarolli LH, Pereira DF, Kappel VD, et al. (2013). Insulin signalling: a potential pathway for the stimulatory effect of kaempferitrin on glucose uptake in skeletal muscle. European Journal of Pharmacology. https://pubmed.ncbi.nlm.nih.gov/23458067/
  6. Garofolo IC, Santos PF, Silva MF, et al. (2026). Kaempferitrin modulates AMPK phosphorylation and PEPCK expression in the liver after a short-term high-fat, high-sucrose diet in mice. Nutrition and Health. https://pubmed.ncbi.nlm.nih.gov/40390681/
  7. Zhu X, Pan Y, Xu X, et al. (2023). Kaempferitrin alleviates LPS-induced septic acute lung injury in mice through downregulating the NF-κB pathway. Allergologia et Immunopathologia. https://pubmed.ncbi.nlm.nih.gov/37937489/
  8. Wang J, Zhao Q (2019). Kaempferitrin inhibits proliferation, induces apoptosis and ameliorates inflammation in rheumatoid-arthritis fibroblast-like synoviocytes. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/31155798/
  9. Li J, Yang J, Xian Q, et al. (2024). Kaempferitrin attenuates unilateral-ureteral-obstruction-induced renal inflammation and fibrosis by inhibiting NOX4-mediated tubular ferroptosis. Phytotherapy Research. https://pubmed.ncbi.nlm.nih.gov/38487990/
  10. Alonso-Castro AJ, Ortiz-Sánchez E, García-Regalado A, et al. (2013). Kaempferitrin induces apoptosis via the intrinsic pathway in HeLa cells. Journal of Ethnopharmacology. https://pubmed.ncbi.nlm.nih.gov/23211658/
  11. Su M, Li Z, Zhou S, et al. (2023). Kaempferitrin, a major compound from the ethanol extract of Chenopodium ambrosioides (epazote), exerts antitumour and hepatoprotective effects in mice with human liver-cancer xenografts. Journal of Pharmacy and Pharmacology. https://pubmed.ncbi.nlm.nih.gov/37203217/
  12. Yang XW, Zhang JY, Xu W, et al. (2005). The biotransformation of kaempferitrin by human intestinal flora. Acta Pharmaceutica Sinica. https://pubmed.ncbi.nlm.nih.gov/16268506/
  13. HATTORI S (1951). Identity of lespedin with kaempferitrin. Nature. https://pubmed.ncbi.nlm.nih.gov/14882347/
  14. Jiang W, Wang R, Liu D, et al. (2018). Protective effects of kaempferitrin on advanced-glycation-end-product-induced mesangial-cell apoptosis and oxidative stress. International Journal of Molecular Sciences. https://pubmed.ncbi.nlm.nih.gov/30373106/